| Bioactivity | BML-277 is a selective checkpoint kinase 2 (Chk2) inhibitor with an IC50 of 15 nM. | ||||||||||||
| Invitro | BML-277 is an ATP-competitive inhibitor of Chk2 that dose dependently protects human CD4+ and CD8+ T-cells from apoptosis due to ionizing radiation. BML-277 efficiently rescues both T-cell populations from radiation-induced apoptosis in a dose-dependent manner with an observed EC50 of 3−7.6 μM. The concentration of BML-277 required for radioprotection is consistent with the biochemical measurement of chk2 inhibition. Providing theKm of ATP for Chk2 is determined to be 99 μM and the Ki for BML-277 is 37 nM, and assuming that the intracellular ATP concentration is 10 mM, a 5 μM concentration of BML-277 would be expected to produce 42% inhibition of intracellular chk2[1]. | ||||||||||||
| Name | BML-277 | ||||||||||||
| CAS | 516480-79-8 | ||||||||||||
| Formula | C20H14ClN3O2 | ||||||||||||
| Molar Mass | 363.80 | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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